A variety of anti-inflammatory medications are prescribed to counteract pain and inflammation associated with a variety of disease states (e.g., rheumatoid arthritis). Commonly prescribed anti-inflammatory medications are generally divided into two mechanism-based groups: cyclooxygenase (COX)-1 inhibitors and COX-2 inhibitors. COX-1 inhibitors, as a class, induce gastric irritation when administered in commercial tablet or capsule dosage forms. COX-2 inhibitors cause much less gastric irritation, but may not affect platelet aggregation to the same extent as COX-1 inhibitors. Additional anti-inflammatory medications include disease-modifying anti-rheumatic drugs (DMARDs) (e.g., methotrexate and dihydrofolate inhibitors), agents that block, absorb, or eliminate excessive tumor necrosis factor (TNF)-α expression or activity, and/or agents that have as a part of their pharmacology an anti-histamine activity (e.g., an H-1 antihistamine).
A variety of medications, while demonstrating efficacy in treating or ameliorating the symptoms of a disease, have a side effect of gastrotoxicity, nephrotoxicity, or hepatotoxicity. For example, several non-steroidal anti-inflammatory drugs (NSAIDs) have been shown to induce gastrotoxicity, nephrotoxicity, or hepatotoxicity following sustained use. As a variety of disease states in humans involve inflammation and/or pain, additional and, preferably, enhanced anti-inflammatory agents and therapies are desired. In fact, virtually all chronic diseases have a component (co-morbidity) of inflammation that sustains and in some cases increases the symptoms of the disease state.
Omega-3 oils have been generally accepted by the health care community as a dietary supplement for the treatment of heart disease and hyperlipidemia. The dose strength and formulation for omega-3 oil required for optimal clinical benefit has yet to be fully defined, but initial studies indicate that the dose necessary to achieve a health benefit was less than 3 grams per day. The American Heart Association recommended dose is 1.0 gram a day and the Food and Drug Administration recommends a maximum daily consumption of omega-3 oil of less than 3.0 grams a day. Omega-3 oils have also been reported to have anti-inflammatory activity. However, the published results regarding this activity are variable and inconsistent. For example, one study reported that administration of omega-3 oil in a dosage of 8 grams a day for 5 months results in a 33-68% decrease in inflammation (Kremer et al., Arthritis Rheum., 38:1107-1114, 1995). In contrast, another study reported that the administration of 2.1 grams of omega-3 oil a day for 8 months mediated only a 12-17% reduction in inflammation (Adam et al., Rheumatoid Int. 23:27-36, 2003). Further studies using gel cap formulations of omega-3 oil in varying dosage strengths were inconclusive or negative. New studies with optimal formulations are required to understand the medical value of omega-3 oil alone and in combination with modern therapeutics.
This patent teaches the use of high dose (greater than 3.0 grams/day) liquid omega-3 oils as an anti-inflammatory therapy. It is difficult to ingest enough gel capsules to achieve this dosage. Compliance and swallowing difficulties limit the ability of many patients to consistently take an amount of omega-3 oil sufficient to elicit an anti-inflammatory effect.
In view of the large number of diseases that involve inflammation and pain, additional anti-inflammatory therapies are desired, and preferably, such therapies do not have negative side effects, such as drug-induced gastrotoxicity, nephrotoxicity, or hepatotoxicity.